Smoothened Receptors
Smoothened (Smo) receptors are non-classical G-protein-coupled receptors that belong to the Frizzled family. Smoothened receptors lack the ability to directly interact with their endogenous ligand, Hedgehog (Hh). In the resting state, Smo receptors are bound to patched (Ptc).
Smoothened Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 7807 | Hh-Ag1.5 |
| Potent and high affinity Smo receptor agonist | |
| 4551 | Purmorphamine |
| Smo receptor agonist | |
| 4366 | SAG |
| Potent Smoothened receptor agonist; activates the Hedgehog signaling pathway | |
| 6390 | SAG dihydrochloride |
| Dihydrochloride salt of SAG; Smo receptor agonist | |
Smoothened Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 1623 | Cyclopamine |
| Inhibitor of Hedgehog (Hh) signaling; Smo antagonist | |
| 5554 | IHR 1 |
| Potent Smo antagonist | |
| 5981 | Itraconazole |
| SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623) | |
| 6538 | PF 04449913 maleate |
| Potent Smo antagonist | |
| 5262 | PF 5274857 hydrochloride |
| High affinity and selective Smoothened (Smo) receptor antagonist | |
| 1974 | SANT-1 |
| Inhibitor of Hedgehog (Hh) signaling; antagonizes smoothened activity | |
| 7826 | Sonidegib |
| Potent Smoothened receptor antagonist | |
Other |
|
| Cat. No. | Product Name / Activity |
| 4474 | 20(S)-Hydroxycholesterol |
| Allosteric activator of Hedgehog signaling; induces Smo accumulation | |
Smoothened (Smo) receptors are non-classical G-protein-coupled receptors that belong to the Frizzled family. Smoothened receptors lack the ability to directly interact with their endogenous ligand, Hedgehog (Hh). In the resting state, Smo receptors are bound to and repressed by patched (Ptc).
Upon Hh-Ptc interaction, Smo receptors are liberated and phosphorylated (activated). This initiates a signaling cascade that controls the activity of transcription factors belonging to the Gli family (particularly Cubitus interruptus (Ci)). Smo receptors are vital for embryogenesis (segmentation and appendage development) and are involved in maintenence of tissue homeostasis in adults. The human gene encoding the Smo receptor has been localized on chromosome 7q32.3.
External sources of pharmacological information for Smoothened Receptors :
Literature for Smoothened Receptors
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